http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-118082-A1
Outgoing Links
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|---|---|
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| filingDate | 2020-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_00a4a6563016ce6c31a470c4ef37c457 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bee7f163f285e5e8ceab1396828e5035 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_609b2c2edc727d61aa7a58dcdbc6368d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6dd36b5ff97fcd098a3f14629e7b763a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9c6b120fa700425adecc6842911d8f3c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_86b1ac370d0e471f20f9a99452494729 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c02db2d110e1312987a7c005afd311c7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a15ddcf006c7c8d22c7c35c2f1e16ba http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d4c918ce4dee9f9ae8186b0e45853091 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fee9f09e31f96f58a239d0d4faea1d38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_420e5302d6a066338106fd4840893086 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_48eb2a3aec7448463b46b870ad8e17b7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32d1b994b6b2bb261dbf577fc020d155 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f11f72adaf5d7ae497affc64601134ae http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_01a3a4d03fedf8e4adc82b931762ccd1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8de8cef58055d07e990426c446d2aac1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_544d0278dcd0040fa297957bf02415e2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f7b4c36b385f1cd596fb4730067b647b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f0c24a7db49f0eebaa831771da22946e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cf5a79fc87edb14a6cc2553ac8d720ec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a5565a2af85dff6ee6d85ef1d2a0c9b1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ad2e3015243b278a275d9c2efa51bbca http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5a9d0d7d5ab5b2e90a77b676b7a910d3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d34db6550697ac06e8ead45c74735d02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_29fe0b30e5ca6091edfa4ca075b2e034 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fa743a31e1e674622682c393b679e4ca http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc1941148ad121d18e28fe4e56bf93e3 |
| publicationDate | 2021-09-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-118082-A1 |
| titleOfInvention | ENZYME INHIBITORS |
| abstract | The present provides compounds of formula (1), compositions comprising said compounds; the therapeutic use of each of said compounds and methods of treatment in patients with each of said compounds; where A, Y, n, R¹, R²A, R²B, R³ and * 1 are defined hereinbefore. Claim 1: A compound of formula (1), wherein * 1 denotes a chiral center; n = 0, 1 or 2; A is selected from H, - (C = O) R⁴, -SO₂R⁶, and - (CH₂) -R¹³; Y is a bond or - [CHR⁵] -; R¹ is H or alkylᵇ; R²A is selected from H, alkyl, - (CH₂) ₀₋₃aryl, - (CH₂) ₀₋₃heteroaryl, - (CH₂) ₀₋₃cycloalkyl, - (CH₂) ₀₋₃- [benzothiophene], - (CH₂) ₀₋ ₃- [indole], and a residue of formula (3); or, when Y is a bond, R¹ and R²A, together with the nitrogen atom to which R¹ is attached and the carbon atom to which R²A is attached, may be attached via alkylene to form a saturated heterocycle of 4, 5, or 6 members, where optionally the 4-, 5-, or 6-membered saturated heterocycle can be substituted with aryl or where two adjacent carbon atoms on the 4-, 5-, or 6-membered saturated heterocycle can be joined to form a 6-membered aromatic ring , or where two adjacent carbon atoms in the 4-, 5-, or 6-membered saturated heterocycle may be joined to form a 3-, 4-, or 5-membered saturated hydrocarbon ring which may be optionally mono- or disubstituted by alkylᵇ; when Y is - [CHR⁵] -, R⁵ is H; or, when Y is - [CHR⁵] -, together with the carbon atoms to which R⁵ and R²A are each attached, R⁵ and R²A may be attached via alkylene to form a saturated 4-, 5- and 6-membered ring; or, when Y is - [CHR⁵] -, together with the nitrogen atom to which R¹ is attached, the carbon atom to which R⁵ is attached, and the carbon atom to which both R²A and R²B are attached, R⁵ and R¹ they may be attached via alkylene to form a saturated 4-, 5-, and 6-membered heterocycle, where optionally one atom in the saturated 4-, 5-, or 6-membered heterocycle may be attached via alkylene to link R²A; R²B is H or alkylᵇ; or, R²A and R²B, together with the carbon to which both R²A and R²B are attached, may be attached via alkylene or heteroalkylene to form a 3, 4, 5, and 6-membered saturated ring, where optionally the 3-membered saturated ring, 4, 5 or 6 members contains one or two ring members selected from N and O; R³ is: (i) a 6.5 or 6.6 fused bicyclic ring, containing a heteroatom selected from S and N, wherein at least one of the rings is aromatic and optionally the bicyclic ring contains an additional heteroatom independently selected from N, O, and S; wherein optionally the fused 6.5 or 6.6 bicyclic ring may be substituted with 1, 2 or 3 substituents selected from alkylᵇ, alkoxy, OH, NH₂, halo, CN, and CF₃; wherein the fused 6.5 bicyclic ring can be attached via the 6 or 5 membered ring; or (ii) phenyl, pyridyl or thiophenyl, which may be optionally substituted with 1, 2 or 3 substituents independently selected from alkylᵇ, alkoxy, OH, NH₂, halo, CN, CF₃, -C (= NH) NH₂, and heteroarylᵇ; wherein when n = 1, and R³ is phenyl substituted with at least - (CH₂NH₂), R²A is alkyl and R²B is H; or (iii) a compound of formula (4); R⁴ is one of: (i) a group of formula (2), where - [L] - is a bond, - [(CH₂) ₁₋₄] -, - [(CH₂) -O- (CH₂)] -, or - [O- (CH₂)] -; and P is alkoxy, OH or NR¹¹R¹²; where * 2 denotes a chiral center, and where when - [L] - is a bond, B is a straight or branched chain C₁₋₄ hydrocarbon, and where when - [L] - is - [(CH₂) ₁₋₄] -, - [(CH₂) -O- (CH₂)] -, or - [O- (CH₂)] -, B is OH, aryl heteroaryl heterocyclyl, cycloalkyl or a moiety of formula (5); or, (ii) - (CH₂) ₘ- [fused 6.5 or 6.6 heteroaromatic bicyclic ring], wherein at least one ring atom is a heteroatom selected from O, N, or S, and optionally, 1,2 or 3 additional ring atoms can be selected from N or NH; wherein the fused 6.5 or 6.6 heteroaromatic bicyclic ring may be optionally substituted with 1, 2, or 3 substituents independently selected from alkylᵇ; wherein the 6.5 heteroaromatic bicyclic ring can be attached to - (CH₂) ₘ- through the 6- or 5-membered ring; or, (iii) methyl, -C (CH₃) ₂ (OH), -C (CH₃) ₂ (NHMe), - (CH₂) ₘ- (aryl), - (CH₂) ₘ- (cycloalkyl), - (CH₂ ) ₘ- (heteroaryl), - (CH₂) ₘ- (heterocyclyl), - (CH₂) - (alkyl), - (CH (halo) ₂), - (CH₂) ₘ- (NR⁸R⁹), - (CH₂) ₘ - (NR¹⁰R⁷), - (CH₂) ₘ-O- (CH₂) ₖ- (aryl), - (CH₂) ₘ- (SO₂) - (CH₂) ₖ- (aryl), - (CH₂) ₘ- (alkoxy) , - (CH₂) ₘ-O- (CH₂) ₖ- (heteroaryl), or - (CH₂) ₘ- [pyridone, which may be optionally substituted by alkylᵇ, or CF₃]; where k = 0, 1, 2 or 3; where m = 0, 1, 2 or 3; where: when Y is - [CHR⁵] - and R⁵ is H, R²A is CH₂aryl or H; and when Y is - [CHR⁵] -, R³ is a moiety of formula (6); when A is H, R³ is the remainder of formula (6); and when R³ is a compound of formula (7), R²A is not H; where: R⁶ is alkyl or - (CH₂) ₀₋₃- (aryl); R⁷ is independently selected from H, -SO₂CH₃, methyl, ethyl, propyl, isopropyl, and cycloalkyl; R⁸ and R⁹ are independently selected from H, -SO₂CH₃, alkylᵇ, heteroarylᵇ, and cycloalkyl; or R⁸ and R⁹ together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, or 7-membered carbon-containing heterocyclic ring, optionally containing an additional heteroatom selected from N, NR¹⁰, S, and O, which it can be saturated or unsaturated with 1 or 2 double bonds and which can be optionally mono or disubstituted with substituents independently selected from oxo, alkylᵇ, alkoxy, OH, halo, -SO₂CH₃, and CF₃; or R⁸ and R⁹ together with the nitrogen atom to which they are attached form a 5- or 6-membered carbon-containing heterocyclic ring, which is fused to an arylᵇ or a heteroarylᵇ; R¹⁰ is independently selected from H, -SO₂R⁶, alkylᵇ, - (CH₂) ₀₋₃arylᵇ, - (CH₂) ₀₋₃heteroarylᵇ, cycloalkyl- (C = O) - (aryl), and - (CH₂) ₀₋₃heterocyclylᵇ; or R¹⁰ is a 4-, 5-, 6-, or 7-membered carbon-containing heterocyclic ring, optionally containing an additional heteroatom selected from N, NR⁷, S, SO, SO₂, and O, which may be saturated or unsaturated with 1 or 2 double bonds and which may be optionally mono or disubstituted with substituents independently selected from oxo, alkylᵇ, alkoxy, OH, halo, -SO₂CH₃, and CF₃; R¹¹ and R¹² are independently selected from H, alkylᵇ, -SO₂R⁶, cycloalkyl - (C = O) O- (alkylᵇ), - (C = O) -phenyl, -CH₂-phenyl, and CH₂-COOH; or R¹¹ and R¹² together with the nitrogen atom to which they are attached form a 4, 5, 6, or 7-membered carbon-containing heterocyclic ring optionally containing an additional heteroatom selected from N, O, and NR¹⁰, wherein the heterocyclic ring may be optionally mono or disubstituted with substituents independently selected from alkylᵇ, OH, halo, and CF₃; R¹³ is selected from heteroaryl cycloalkyl heterocyclyl and arylᵇ; wherein: alkoxy is an O-linked linear hydrocarbon of 1 to 6 carbon atoms (C₁₋₆) or an O-linked branched hydrocarbon of 3 to 6 carbon atoms (C₃₋₆); alkoxy can be optionally substituted with 1 or 2 substituents independently selected from OH, CN, CF₃, -N (R⁷) ₂, and fluoro; alkyl is a linear saturated hydrocarbon having up to 6 carbon atoms (C₁₋₆) or a branched saturated hydrocarbon having between 3 and 6 carbon atoms (C₃₋₆); alkyl can be optionally substituted with 1 or 2 substituents independently selected from C₁₋₆alkoxy, OH, -NR⁸R⁹, -NHCOCH₃, -CO (heterocyclylᵇ), -COOR⁸, -CONR⁸R⁹, CN, CF₃, halo, oxo and heterocyclylᵇ; alkylᵇ is a linear saturated hydrocarbon having up to 6 carbon atoms (C₁₋₆) or a branched saturated hydrocarbon having between 3 and 6 carbon atoms (C₃₋₆); alkyl can be optionally substituted with 1 or 2 substituents independently selected from C₁₋₆alkoxy, OH, -N (R⁷) ₂, -NHCOCH₃, CF₃, halo, oxo, and cyclopropane; alkylene is a divalent linear saturated hydrocarbon having 1 to 5 carbon atoms (C₁₋₅); alkylene can be optionally substituted with 1 or 2 substituents independently selected from alkyl, C₁₋₆alkoxy, OH, CN, CF; and halo; aryl is phenyl, biphenyl, or naphthyl; aryl may be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, OH, -SO₂CH₃, halo, -SO₂NR⁸R⁹, CN, - (CH₂) ₀₋₃-O-heteroarylᵇ, arylᵇ, -O-arylᵇ , - (CH₂) ₀₋₃-heterocyclylᵇ, - (CH₂) ₁₋₃-arylᵇ, - (CH₂) ₀₋₃-heteroarylᵇ, -COOR⁸, -CONR⁸R⁹, - (CH₂) ₀₋₃-NR⁸R⁹, OCF₃ and CF₃ ; or two adjacent carbon ring atoms therein may be optionally linked by a heteroalkylene to form a non-aromatic ring containing 5, 6, or 7 ring members which may be optionally substituted with OH; or wherein optionally two adjacent ring atoms in the aryl are joined to form a 5- or 6-membered aromatic ring containing 1 or 2 heteroatoms selected from N, NR¹⁰, S, and O; arylᵇ is phenyl, biphenyl, or naphthyl, which may be optionally substituted with 1, 2, or 3 substituents independently selected from methyl, ethyl, propyl, isopropyl, alkoxy, OH, -SO₂CH₃, N (R⁷) ₂, halo, CN, and CF₃ ; or two adjacent ring carbon atoms in the aryl may optionally be linked by a heteroalkylene to form a non-aromatic ring containing 5, 6, or 7 ring members; cycloalkyl is a monocyclic saturated hydrocarbon ring of 3 to 6 carbon atoms (C₃₋₆); cycloalkyl can be optionally substituted with 1 or 2 substituents independently selected from methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, OH, CN, CF₃, and halo; wherein optionally two adjacent ring atoms in the cycloalkyl are joined to form a 5- or 6-membered saturated hydrocarbon ring; halo is F, Cl, Br, or I; heteroalkylene is a divalent linear saturated hydrocarbon having 2 to 5 carbon atoms (C₂₋₅), where 1 or 2 of the 2 to 5 carbon atoms are replaced with NR¹⁰, S or O; heteroalkylene can be optionally substituted with 1 or 2 substituents independently selected from alkyl, C₁₋₆alkoxy, OH, CN, CF₃, and halo; heteroaryl is a 5- or 6-membered carbon-containing aromatic ring containing one, two, or three ring members selected from N, NR¹⁰, S, and O; heteroaryl may be optionally substituted with 1, 2, or 3 substituents independently selected from alkyl, alkoxy, heteroarylᵇ, phenyl, cycloalkyl, OH, OCF₃, halo, heterocyclylᵇ, CN, and CF₃; heteroarylᵇ is a 5- or 6-membered carbon-containing aromatic ring containing one, two, or three ring members selected from N, NR¹⁰, S, and O; heteroarylᵇ can be optionally substituted with 1, 2 or 3 substituents independently selected from methyl, ethyl, propyl, isopropyl, alkoxy, OH, OCF₃, COOCH₃, COOCH₂CH₃, COO- (CH₂) ₂-CH₃, COO- (iPr), halo, CN, and CF₃; heterocyclyl is a 4-, 5-, 6-, or 7-membered non-aromatic carbon-containing ring containing one, two, three, or four ring members selected from N, NR¹⁰, S, SO, SO₂, and O; heterocyclyl can be optionally substituted with 1, 2, 3, or 4 substituents independently selected from alkyl, alkoxy, arylᵇ, OH, OCF₃, halo, oxo, CN, NR⁸R⁹, -O (arylᵇ), -O (heteroarylᵇ) and CF₃ ; or wherein optionally two ring atoms in the heterocyclyl are bonded with an alkylene to form a non-aromatic ring containing 5, 6, or 7 ring members; or wherein optionally two ring atoms in the heterocyclyl are linked with a heteroalkylene to form a non-aromatic ring containing 5, 6 or 7 ring members; or wherein optionally two adjacent ring atoms on the heterocyclyl are joined to form a 5- or 6-membered aromatic ring which may optionally contain 1 or 2 heteroatoms selected from N, NR¹⁰, S, and O; heterocyclylᵇ is a 4, 5, 6, or 7-membered carbon-containing non-aromatic ring containing one, two, or three ring members selected from N, NR⁷, S, SO, SO₂, and O; heterocyclylᵇ can be optionally substituted with 1, 2, 3, or 4 substituents independently selected from methyl, ethyl, propyl, isopropyl, alkoxy, OH, OCF₃, halo, oxo, CN, and CF₃; and tautomers, isomers, stereoisomers (including enantiomers, diastereoisomers, and racemic and non-racemic mixtures thereof), deuterated isotopes, and pharmaceutically acceptable sales and / or solvates thereof. |
| priorityDate | 2019-08-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 103.